产品
编 号：F627268
分子式：C24H25N3O2
分子量：387.47
分子式：C24H25N3O2
分子量：387.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 1160852-22-1
产品详情
生物活性：
S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 μM. S130 suppresses autophagy flux.
体内研究：
S130 (20 mg/kg; i.p.; daily; 3 weeks) suppresses tumor growth, and shows an efficient in vivo antitumor effect with a sound safety on vital organs.Animal Model:BALB/c nude female mice (4 weeks), with HCT116 cells xenograft
Dosage:20 mg/kg
Administration:Intraperitoneal injection; daily; 3 weeks
Result:Was able to suppress tumor growth and with a sound safety on vital organs.
体外研究：
S130 suppresses autophagy and activates apoptosis by inhibiting ATG4B, leads to enhanced cytotoxicity.S130 (10 μM; 6 hours) suppresses autophagy at the early LC3 priming step or late autolysosome degradation stage.S130 accumulates autolysosomes with more lipidated LC3.S130 (0-25 μM; 48 hours) induces cell death through inhibiting the activity of ATG4B at a dose higher than 6.3 μM. And such cytotoxicity might not cause cell death through necroptosis.Nutrient deprivation enhances S130-induced cytotoxicity.S130 (0-10μM; 24 hours) suppresses approximately 79% of the cleavage of full-length LC3-GST at the 10 μM, while no substrates were processed in ATG4B KO cells. S130 displays obvious inhibitory effects on ATG4B.
S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 μM. S130 suppresses autophagy flux.
体内研究：
S130 (20 mg/kg; i.p.; daily; 3 weeks) suppresses tumor growth, and shows an efficient in vivo antitumor effect with a sound safety on vital organs.Animal Model:BALB/c nude female mice (4 weeks), with HCT116 cells xenograft
Dosage:20 mg/kg
Administration:Intraperitoneal injection; daily; 3 weeks
Result:Was able to suppress tumor growth and with a sound safety on vital organs.
体外研究：
S130 suppresses autophagy and activates apoptosis by inhibiting ATG4B, leads to enhanced cytotoxicity.S130 (10 μM; 6 hours) suppresses autophagy at the early LC3 priming step or late autolysosome degradation stage.S130 accumulates autolysosomes with more lipidated LC3.S130 (0-25 μM; 48 hours) induces cell death through inhibiting the activity of ATG4B at a dose higher than 6.3 μM. And such cytotoxicity might not cause cell death through necroptosis.Nutrient deprivation enhances S130-induced cytotoxicity.S130 (0-10μM; 24 hours) suppresses approximately 79% of the cleavage of full-length LC3-GST at the 10 μM, while no substrates were processed in ATG4B KO cells. S130 displays obvious inhibitory effects on ATG4B.
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